Middleeast Pharmacy and Pharmaceutical conference

One of the major unsolved problems in pharmaceutical drug development is the poor water solubility of many active pharmaceutical ingredients (APIs) and hence reduced bioavailability. Researchers have attempted to minimize the

problem by reducing the drug particle size. While, many of these platforms bring unique advantages to the field of drug delivery, an ideal solution would be to remove the problem of solubility entirely, by reducing the API size to clusters of a few molecules, bound by weak, Van der Waal’s forces that would readily dissociate into molecules, during enteral or parenteral drug delivery process. In order to have commercial impact, such molecular clusters should also be produced in sufficiently high yield. We have precipitated molecular clusters of two drug molecules, ibuprofen and naproxen, respectively, via supersonic jet expansion of the supercritical CO2 drug formulation into a collection vessel cooled to liquid N2 temperatures and capturing the clusters instantaneously in dry ice with up to 80% yield. Gradual dissolution of the dry ice in water, at room temperature, resulted in the true solubilization of these clusters. Drop casting and ambient drying of the solution on a substrate (e.g. silicon) resulted in a stable, viscous liquid film, which we refer to as a nanostructured molecular liquid. This is a significant observation, considering the fact that, normally, ibuprofen and naproxen are solid powder at room temperature and pressure, with melting points of 76 ºC and 154 ºC, respectively. In vitro cancer cell viability studies of water-solubilized ibuprofen and naproxen exhibit similar cytotoxicity to that of the original raw materials, thus retaining their potency. Besides its scientific importance, this invention is expected to open up new drug delivery platforms.